RS54723B1 - Kondenzovani derivati imidazola koji su korisni kao ido inhibitori - Google Patents

Kondenzovani derivati imidazola koji su korisni kao ido inhibitori

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Publication number
RS54723B1
RS54723B1 RS20160285A RSP20160285A RS54723B1 RS 54723 B1 RS54723 B1 RS 54723B1 RS 20160285 A RS20160285 A RS 20160285A RS P20160285 A RSP20160285 A RS P20160285A RS 54723 B1 RS54723 B1 RS 54723B1
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6alkyl
alkyl
membered heterocycle
heteroaryl
cyano
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Mario Mautino
Sanjeev Kumar
Jesse Waldo
Firoz Jaipuri
Tanay Kesharwani
Xiaoxia Zhang
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Newlink Genetics Corporation
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Publication of RS54723B1 publication Critical patent/RS54723B1/sr

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Abstract

Jedinjenje formule,ili njegova farmaceutski prihvatljiva so, pri čemuveza α je jednostruka ili dvostruka veza;n je 0, 1, 2, 3, ili 4;svaki R1 je nezavisno halogen, cijano, nitro, C1-6alkil, C1-6haloalkil, -OR, - N(R)2, -SR, -C(O)OR, -C(O)N(R)2, -C(O)R, -S(O)R, -S(O)OR, -S(O)N(R)2, -S(O)2R, -S(O)2OR, -S(O)2N(R)2, -OC(O)R, -OC(O)OR, -OC(O)N(R)2, -N(R)C(O)R, -N(R)C(O)OR, ili -N(R)C(O)N(R)2;R2 je -C1-4 alkil-RA ili -C2-4alkenil-R3 kada je veza α jednostruka veza; iR2 je =C(H)RA kada je veza a dvostruka veza;pri čemuRA je -CN, -C(O)R3, -C(O)OR3, -C(O)N(R3)(Rc), -C(ORB)(R3)(Rc), -C(NHRB)(R3)(RC), ili -C(=N-ORc)R3,pri čemuRB jevodonik, C1-6alkil, C1-6haloalkil, - C1-6alkil-RB1, -C(O)R3, -C(O)N(H)R3 ili -S(O)2R3, -C(O)(CH2)1-4COOR, -C(O)(CH2)i-4(NR)COOR, -C(O)CH(NH2)(RD), -S(O)2OR3, -S(O)2N(R3)2, -CH2-OP(O)2(OR)2, ili -P(O)(OR3)2, pri čemuRB1 je cijano, nitro, C1-6alkil, C1-6haloalkil, -OR, -N(R)2, -SR, -C(O)OR, -C(O)N(R)2, -C(O)R, -S(O)R, -S(O)OR, -S(O)N(R)2, -S(O)2R, -S(O)2OR, -S(O)2N(R)2, -OC(O)R, -OC(O)OR, -OC(O)N(R)2, -N(R)C(O)R, -N(R)C(O)OR, ili -N(R)C(O)N(R)2;RD je vodonik, metil, -CH(CH3)2, -CH2CH(CH3)2, -CH(CH3)(CH2CH3), benzil, 4-hidroksibenzil, -CH2(3-indolil), -CH2SH, -CH2CH2SCH3, -CH2OH, -CH(CH3)OH, -(CH2)4-NH2, -(CH2)3-N(H)C(=NH)NH2, -CH2(4-imidazolil), -CH2COOH, -CH2CH2COOH,-CH2CONH2, -CH2CH2CONH2;svaki R3 je nezavisno vodonik, C1-6alkil, C1-6haloalkil, aril, heteroaril, C3-8cikloalkil, C3-8 cikloalkenil, 3-10-člani heterocikl, arilC1-6alkil-, heteroaril C1-6alkil-, C3-8cikloalkil C1-6alkil-, C3-8cikloalkenilC1-6 alkil-, (3-10-člani heterocikl)C1-6 alkil-, ili (heteroaril)-(3-10-člani heterocikl)-,pri čemu sualkil, C3-8cikloalkil, C3-8cikfoalkenii, 3-10-člani heterocikl, C3-8cikloalkil C1-6alkil-, C3-8cikloalkenil C1-6alkil-, (3-10-čiani heterocikl) C1-6alkil-, i (heteroaril)-(3-10-člani heterocikl)-, svi opciono i nezavisno zamenjeni jednom =R32 grupom i svaki je opciono i nezavisno supstituisan sa jednom, dve, tri ili četiri R31 grupe;aril, heteroaril, arilC1-6alkil-, i heteroarilC1-6alkil- grupe, su sve opciono zamenjene sa jednom, dve, tri ili četiri R31 grupe;pri čemusvaki R31 je nezavisno halogen, cijano, nitro, C1-6alkil, - C1-6alkil-R33, C1-6haloalkil, -OR, -N(R)2, -SR, -C(O)OR, -C(O)N(R)2, -C(O)N(OH)R, -C(O)R, -C(NR11)R, -C(NR11)N(R11)R, ~S(O)R, -S(O)OR, -S(O)N(R)2, -S(O)2R, -S(O)2OR, -S(O)2N(R)2, -OC(O)R, -OC(O)OR, -OC(O)N(R)2, -N(R)C(O)R, -N(R)C(O)OR, -N(R)C(O)N(R)2, pri čemuR33 je cijano, -OR, -N(R)2, -SR, -C(O)OR, -C(O)N(R)2, -C(O)R, -S(O)R, -S(O)OR, -S(O)N(R)2, -S(O)2R, -S(O)2OR, -S(O)2N(R)2, -OC(O)R, -OC(O)OR,-OC(O)N(R)2, -N(R)C(O)R, -N(R)C(O)OR, ili -N(R)C(O)N(R)2;R32 je =O, =S, =N(R), =N(OR), =C(R34)2, =(spiro-C3-8 cikioalkil), ili =(spiro-(3-10-člani heterocikl)),pri čemusvaki R34 je nezavisno vodonik, halogen, cijano, C1-6alkil, - C1-6alkil-OR, C1-6haloalkil, C3-8cikloalkil, iii 3-10-člani heterocikl;ili oba R34 uzeta zajedno sa atomom za koji su oba vezana obrazujumonociklični C3-8 cikloalkil ili monociklični 3-8-člani heterocikl;Rc je vodonik ili C1-6alkil;isvaki R je nezavisno vodonik ili R10, pri čemuR10 je C1-6alkii, C1-6haloalkii, aril, heteroaril, C3-8cikloalkil, C3-8cikloalkenil, 3-10-člani heterocikl, arilC1-6alkil, heteroaril C1-6alkil-, C3-8cikioalkil C1-6alkil-, C3-8cikioalkenil C1-6alkil-, ili (3-10-člani heterociki) C1-6alkil-, svaki R10 je opciono zamenjen sa jednom, dve, tri ili četiri grupe koje su sve nezavisno halogen, cijano, nitro, C1-6alkil, C1-6haloalkil, -OR11, -N(R11)2, -SR11, -C(O)OR11, -C(O)N(R11)2, -C(O)R11-S(O)R11, -S(O)OR11, -S(O)N(R11)2, -S(O)2R11, -S(O)2OR11, -S(O)2N(R11)2, -OC(O)R11, -OC(O)OR11-OC(O)N(R11)2, -N(R11)C(O)R11, -N(R11)C(O)OR11, -N(R11)C(O)N(R11)2,-N(R11)S(O)2R11, ili -C(O)-(3-10-člani heterocikl). pri čemu je svaki R11 nezavisno vodonik ili C1-6alkil.Prijava sadrži još 20 patentnih zahteva.
RS20160285A 2011-04-15 2012-04-12 Kondenzovani derivati imidazola koji su korisni kao ido inhibitori RS54723B1 (sr)

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US201161475788P 2011-04-15 2011-04-15
PCT/US2012/033245 WO2012142237A1 (en) 2011-04-15 2012-04-12 Fused imidazole derivatives useful as ido inhibitors

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